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Carbazole Scaffold in Medicinal Chemistry and Natural Products: A Review from 2010-2015.
Current Topics in Medicinal Chemistry ( IF 2.9 ) Pub Date : 2015-09-16 , DOI: 10.2174/1568026615666150915112647
Lissa S Tsutsumi , Daniela Gündisch , Dianqing Sun 1
Affiliation  

9H-carbazole is an aromatic molecule that is tricyclic in nature, with two benzene rings fused onto a 5-membered pyrrole ring. Obtained from natural sources or by synthetic routes, this scaffold has gained much interest due to its wide range of biological activity upon modifications, including antibacterial, antimalarial, anticancer, and anti-Alzheimer properties. This review reports a survey of the literature on carbazole-containing molecules and their medicinal activities from 2010 through 2015. In particular, we focus on their in vitro and in vivo activities and summarize structure-activity relationships (SAR), mechanisms of action, and/or cytotoxicity/selectivity findings when available to provide future guidance for the development of clinically useful agents from this template.

中文翻译:

药物化学和天然产物中的咔唑支架:2010-2015年综述。

9H-咔唑是一种本质上为三环的芳族分子,其中两个苯环稠合在5元吡咯环上。从天然来源或通过合成途径获得的支架,由于其修饰后的广泛生物活性而广受关注,包括抗菌,抗疟疾,抗癌和抗阿尔茨海默氏症。这篇综述报告了从2010年到2015年有关含咔唑分子及其药物活性的文献调查。特别是,我们重点研究了它们的体外和体内活性,并总结了结构-活性关系(SAR),作用机理和/或细胞毒性/选择性发现,以便为该模板开发临床上有用的药物提供未来指导。
更新日期:2019-11-01
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